Valuable Biological Activities Research Articles

Antitumor and Protective Effects of Melatonin: The Potential Roles of MicroRNAs.

MicroRNAs (miRNAs) are endogenous short noncoding RNAs with approximately 22 nucleotides. The primary function of miRNAs is the negative regulation of target gene expression via mRNA degradation or translation inhibition. During recent years, much attention has been made toward miRNAs' role in different disorders; particularly cancer and compounds with modulatory effects on miRNAs are of interest. Melatonin is one of these compounds which is secreted by the pineal gland. Also, melatonin is present in the leaves, fruits, and seeds of plants. Melatonin has several valuable biological activities such as antioxidant, anti-inflammation, antitumor, and antiaging activities. This important agent is extensively used to treat different disorders such as cancer and neurodegenerative and cardiovascular diseases. This review aims to describe the modulatory effect of melatonin on miRNAs as novel targets.

A Survey of Synthetic Routes and Antitumor Activities for Benzo[g]quinoxaline-5,10-diones

Anthracycline antibiotics play an important role in cancer chemotherapy. The need to improve their therapeutic index has stimulated an ongoing search for anthracycline analogs with enhanced properties. This review aims to summarize the common synthetic approaches to benzo[g]quinoxaline-5,10-diones and their uses in heterocyclic chemistry. Because of the valuable biological activities of the 1,4-diazaanthraquinone compounds, a summary of the most promising heterocyclic quinones is provided together with their antitumor properties.

Antioxidant activity, total phenolics and flavonoids contents of Pandanus amaryllifolius (Roxb.)

Pandanus amaryllifolius Roxb. was commonly used in Vietnam as a fragrance because of its aroma. These aromatic plants are the primary source of medicinal herbs because of their valuable biological activities. This study was aimed at determining the phytochemical content, Total flavonoids contents (TFC), total phenolic content (TPC) and antioxidants were analyzed by Folin-Ciocalteu and DPPH scavenging assays, respectively. The total flavonoid content is measured by the aluminum chloride method. The qualitative phytochemical analysis confirmed the presence of flavonoids, terpenoids, coumarin, and reducing sugar, which is chemical components in Pandanus amaryllifolius Roxb extract. Results showed that ethanol extract exhibited higher DPPH (129.327 ug/ml) and TPC (38.12 mgGAE/DW) activity than water extraction (265.738 ug/ml and 10.97 mgGAE/DW). Research shows that using this plant more in pharmaceuticals or food should be focused and developed.

Plant Polyphenols: Natural and Potent UV-Protective Agents for the Prevention and Treatment of Skin Disorders.

Nowadays, destructive and immunosuppressive effects from long-term exposure to UV radiation have been fully investigated and documented in the literature. UV radiation is known as the main cause of skin aging and carcinogenesis. Hence, skin protection against anti-oxidative and immunosuppressive processes is highly in demand. Now, plant polyphenols have been found as a versatile and natural tool for the prevention and treatment of various skin diseases. The presence of a large number of hydroxyl groups in the cyclic structure of polyphenols has induced valuable biological activities. Among them, their UV protective activity has attracted lots of attention due to promising efficacy and simple instruction to use.

Resveratrol, a Molecule with Anti-Inflammatory and Anti-Cancer Activities: Natural Product to Chemical Synthesis.

Resveratrol, a natural polyphenol product, is used in plant defense from fungal and microbial aggression. It is found naturally, especially in plants such as grapes, peanuts, and berries. It has the highest concentrations in blueberries, mulberries, blackberries, and the skin of red grapes. Resveratrol has various pharmacological properties such as anti-inflammatory, cytoprotective, and antineoplastic activities. We conducted a literature survey using standard tools such as Google, Reaxys, Scifinder, Scihub, and patent Espacenet to compile the biosynthetic pathways, all organic synthetic methods, and biological activities reported for resveratrol till date. More than one hundred research articles and patents were referred to write this review. About twenty-five of them are related to chemical synthesis, and the rests are about the source, pharmacological activity, and other properties of resveratrol. This study reveals that many common pathways are involved in various pharmacological activities, which can be useful for treating various diseases based on the pathways involved. Reactions such as Pfitzner-Moffatt oxidation, Wittig-Horner condensation, Mizoroki-Heck, Perkin, Wittig, etc. have been used in resveratrol synthesis. A structure-activity relationship was also established based on its analogs and derivatives. This review examined and reported all the published biological activities and chemical syntheses of resveratrol apart from the biosynthetic pathway. Due to its valuable biological activities, various synthetic approaches have been reported till date. The reported synthetic operations are suitable for large-scale industrial production. Moreover, these comprehensive synthetic procedures could be utilized in the preparation of stilbenes and other related compounds in future endeavors.

Comparative Analysis of Far East Sikhotinsky Rhododendron (Rh. sichotense) and East Siberian Rhododendron (Rh. adamsii) Using Supercritical CO2-Extraction and HPLC-ESI-MS/MS Spectrometry.

Rhododendron sichotense Pojark. and Rhododendron adamsii Rheder have been actively used in ethnomedicine in Mongolia, China and Buryatia (Russia) for centuries, as an antioxidant, immunomodulating, anti-inflammatory, vitality-restoring agent. These plants contain various phenolic compounds and fatty acids with valuable biological activity. Among green and selective extraction methods, supercritical carbon dioxide (SC-CO2) extraction has been shown to be the method of choice for the recovery of these naturally occurring compounds. Operative parameters and working conditions have been optimized by experimenting with different pressures (300–400 bar), temperatures (50–60 °C) and CO2 flow rates (50 mL/min) with 1% ethanol as co-solvent. The extraction time varied from 60 to 70 min. A HPLC-UV-VIS-ESI-MS/MS technique was applied to detect target analytes. A total of 48 different biologically active components have been identified in the Rh. adamsii SC-CO2 extracts. A total of 31 different biologically active components have been identified in the Rh. sichotense SC-CO2 extracts.

Trio of enzymes power divergent synthesis

Organic Chemistry Diterpene natural products are built from a 20-carbon building block, with a huge range of possible structures and modifications. Chemical synthesis of specific molecules, some of which have valuable biological activities, is tricky because of the need for selective oxidations and rearrangements when starting from widely available scaffolds. Zhang et al. characterized selectivities for three oxidative enzymes that each attack different positions on a common scaffold. They then seamlessly combined chemical transformations with the enzymatic oxidations to produce nine distinct compounds across three families of diterpenes. These results highlight the potential of hybrid organic-biocatalytic synthetic schemes for divergent synthesis. Science , this issue p. [799][1] [1]: /lookup/doi/10.1126/science.abb8271

Metabolite profiling by means of GC-MS combined with principal component analyses of natural populations of Nectaroscordum siculum ssp. bulgaricum (Janka) Stearn.

Nectaroscordum siculum ssp. bulgaricum (Janka) Stearn (Allium siculum subsp. dioscoridis (Sm.) K. Richt.) is a traditional culinary spice from South-East Europe. Studies of N.siculum have focused mainly on the botanical and taxonomic characteristics of this species and there is no data available in the scientific literature about its metabolite profile. Thus, the aim of the current study was metabolite profiling of four wild populations of N.siculum grown in Bulgaria by gas chromatography coupled to mass spectrometry (GC-MS) and subsequent principal component analysis (PCA) of the data obtained. The identified primary metabolites (carbohydrates, amino acids, organic acids and lipids) are initial compounds for the biosynthesis of different plant secondary metabolites, such as polyphenols and flavour compounds with valuable biological activities for humans. The health benefits of the phenolic acids identified in this study have been a prerequisite for the implementation of N.siculum in different food systems in order to increase their quality and biological value.

Evaluation of Phoenix dactylifera Edible Parts and Byproducts as Sources of Phytoprostanes and Phytofurans.

Even though traditionally date-fruit has been featured by a marginal use, mainly restricted to its dietary intake, in recent years, it has raised the range of applications for this agro-food production. These new uses have entailed an enlarged production of date fruits and, simultaneously, of date palm byproducts. Encouraged by the traditional medicinal uses of dates, according to their phytochemical composition, the present work was focused on the evaluation of a new family of secondary metabolites, the plant oxylipins phytoprostanes (PhytoPs) and phytofurans (PhytoFs), in six separate matrixes of the date palm edible parts and byproducts, applying an UHPLC-ESI-QqQ-MS/MS-based methodology. The evaluation for the first time of date palm edible parts and byproducts as a dietary source of PhytoPs and PhytoFs provides evidence on the value of six different parts (pulp, skin, pits, leaves, clusters, and pollen) regarding their content in these plant oxylipins evidenced by the presence of the PhytoPs, 9-F1t-PhytoP (201.3-7223.1 ng/100 g dw) and 9-epi-9-F1t-PhytoP (209.7-7297.4 ng/100 g dw), and the PhytoFs ent-16(RS)-9-epi-ST-Δ14-10-PhytoF (4.6-191.0 ng/100g dw), and ent-16(RS)-13-epi-ST-Δ14-9-PhytoF as the most abundant compounds. Regarding the diverse matrixes assessed, pollen, clusters, and leaves for PhytoPs and skins and pollen for PhytoFs were identified as the most interesting sources of these compounds. In this concern, the information obtained upon the detailed characterization performed in the present work will allow unravelling the biological interest of PhytoPs and PhytoFs and the extent to which these compounds could exert valuable biological activities upon in vitro (mechanistic) and in vivo studies, allocating the effort-focus on the chemical species of PhytoPs and PhytoFs responsible for such traits.

Bioactive Polysaccharides from Seaweeds.

Bioactive compounds with diverse chemical structures play a significant role in disease prevention and maintenance of physiological functions. Due to the increase in industrial demand for new biosourced molecules, several types of biomasses are being exploited for the identification of bioactive metabolites and techno-functional biomolecules that are suitable for the subsequent uses in cosmetic, food and pharmaceutical fields. Among the various biomasses available, macroalgae are gaining popularity because of their potential nutraceutical and health benefits. Such health effects are delivered by specific diterpenes, pigments (fucoxanthin, phycocyanin, and carotenoids), bioactive peptides and polysaccharides. Abundant and recent studies have identified valuable biological activities of native algae polysaccharides, but also of their derivatives, including oligosaccharides and (bio)chemically modified polysaccharides. However, only a few of them can be industrially developed and open up new markets of active molecules, extracts or ingredients. In this respect, the health and nutraceutical claims associated with marine algal bioactive polysaccharides are summarized and comprehensively discussed in this review.

Secondary Metabolites of the Genus Didemnum: A Comprehensive Review of Chemical Diversity and Pharmacological Properties.

Tunicates (ascidians) are common marine invertebrates that are an exceptionally important source of natural products with biomedical and pharmaceutical applications, including compounds that are used clinically in cancers. Among tunicates, the genus Didemnum is important because it includes the most species, and it belongs to the most speciose family (Didemnidae). The genus Didemnum includes the species D. molle, D. chartaceum, D. albopunctatum, and D. obscurum, as well as others, which are well known for their chemically diverse secondary metabolites. To date, investigators have reported secondary metabolites, usually including bioactivity data, for at least 69 members of the genus Didemnum, leading to isolation of 212 compounds. Many of these compounds exhibit valuable biological activities in assays targeting cancers, bacteria, fungi, viruses, protozoans, and the central nervous system. This review highlights compounds isolated from genus Didemnum through December 2019. Chemical diversity, pharmacological activities, geographical locations, and applied chemical methods are described.

Rapid Mass Spectrometric Study of a Supercritical CO2-extract from Woody Liana Schisandra chinensis by HPLC-SPD-ESI-MS/MS.

Woody liana Schisandra chinensis contains valuable lignans, which are phenylpropanoids with valuable biological activity. Among green and selective extraction methods, supercritical carbon dioxide (SC-CO2) was shown to be the method of choice for the recovery of these naturally occurring compounds. Carbon dioxide (CO2) was the solvent with the flow rate (10−25 g/min) with 2% ethanol as co-solvent. In this piece of work operative parameters and working conditions were optimized by experimenting with different pressures (200–400 bars) and temperatures (40–60 °C). The extraction time varied from 60 to 120 min. HPLC-SPD-ESI -MS/MS techniques were applied to detect target analytes. Twenty-six different lignans were identified in the S. chinensis SC-CO2 extracts.

Tangeretin: a mechanistic review of its pharmacological and therapeutic effects.

To date, a large number of synthetic drugs have been developed for the treatment and prevention of different disorders, such as neurodegenerative diseases, diabetes mellitus, and cancer. However, these drugs suffer from a variety of drawbacks including side effects and low efficacy. In response to this problem, researchers have focused on the plant-derived natural products due to their valuable biological activities and low side effects. Flavonoids consist of a wide range of naturally occurring compounds exclusively found in fruits and vegetables and demonstrate a number of pharmacological and therapeutic effects. Tangeretin (TGN) is a key member of flavonoids that is extensively found in citrus peels. It has different favorable biological activities such as antioxidant, anti-inflammatory, antitumor, hepatoprotective, and neuroprotective effects. In the present review, we discuss the various pharmacological and therapeutic effects of TGN and then, demonstrate how this naturally occurring compound affects signaling pathways to exert its impacts.

Cytotoxicity and antioxidant activity of plant extracts from Vietnam

Traditional medicine plays an important role in treatment of human diseases. Extracts from medicinal plants exhibit many valuable biological activities. However, the exploitation and application of the extracts requires knowlege on the mechanism of action. In this study, cytotoxic and antioxidant activites of the methanol and hexane extracts of 09 Vietnamese plants have been studied in vitro on keratinocyte HaCaT cell line. The results showed that all plant extracts had a cytotoxyc effect on HaCaT cells. The hexane extracts showed more potent than the methanol extract. Garcinia mangostana exhibited the best cytotoxicity with IC50 values of 14.42 mg/ml (for hexane extract) và 14.27 mg/ml (for MeOH extract). All tested extracts resulted in the generation of intracellular reactive oxygen radicals in HaCaT cells. Mangifera indica, Cleistocalyx operculatus and Terminalia catappa had the best DPPH radical scavenging activity with EC50 values of 23.0 mg/ml, 27.4 mg/ml and 23.73 mg/ml, respectively. Besides, G. mangostana and T.catappa exhibited capacity of eliminating active oxygen radicals (iROS). The test extracts significantly reduced the number of cells in phase G1 and increased the number of cells in S and G2/M phases. The data obtained in this study are the preliminary results for further studies on the mechanisms of action and therapeutic applications of these plants.

A Comparative Study on Antioxidation and Antibacterial Activities Triphala Herb Extracts from Chae Son, Lampang, Thailand

Introduction: Triphala, a herbal medicine which is a product from Chae Son, Lampang, Thailand, is an unequal-proportional mixture of fruits of three herbs, Phyllanthus emblica, Terminalia chebula, and Terminalia bellirica (2:1:1).
 Materials and Methods: The contemporary study concentrated on extracts detection and comparative analysis between various annual year (A.D.2017/2018) activities in hexane, ethyl acetate, and methanolic extracts of Triphala. The determination of antioxidant was using by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP). The broth dilution and agar well diffusion assay were determined antibacterial.
 Results: Results exposed the valuable biological activity extracts from ethyl acetate and methanol solvents of T. chebula and T. bellirica, which strength is accountable for biological activities. Extracts displayed acceptable radical-scavenging activity analogous with ascorbic acid. The methanol extract of T. bellirica (0.0013 mg/mL), ethyl acetate extract of P. emblica (0.0009 mg/mL), in A.D. 2017 and the ethyl acetate extract of P. emblica (0.0090 mg/mL), the methanol extract of Triphala (0.0176 mg/mL) in 2018, were exhibited higher antioxidant activity. Also, extracts indicated hopeful antibacterial potential against tested strain comparable to chloramphenicol.
 Conclusion: The results in A.D. 2017 showed that inhibition zone of P. emblica in ethyl acetate extract; S. aureas (8.67 mm), E. aerogenes (8.67 mm), E. coli (EPEC) (7.67 mm), P. mirabilis (7.73 mm) , S. typhimurium (8.33 mm), S. flexneri (8.33 mm) and V. cholera (7.33 mm) together with P. emblica methanol extract; S. aureas (6.67 mm), E. aerogenes (7.76 mm.) and V. cholera (4.0 mm). Therefore, it could be concluded that Triphala may be a talented candidate in pharmaceutical and future medicine.

Citrus limon (Lemon) Phenomenon-A Review of the Chemistry, Pharmacological Properties, Applications in the Modern Pharmaceutical, Food, and Cosmetics Industries, and Biotechnological Studies.

This review presents important botanical, chemical and pharmacological characteristics of Citrus limon (lemon)—a species with valuable pharmaceutical, cosmetic and culinary (healthy food) properties. A short description of the genus Citrus is followed by information on the chemical composition, metabolomic studies and biological activities of the main raw materials obtained from C. limon (fruit extract, juice, essential oil). The valuable biological activity of C. limon is determined by its high content of phenolic compounds, mainly flavonoids (e.g., diosmin, hesperidin, limocitrin) and phenolic acids (e.g., ferulic, synapic, p-hydroxybenzoic acids). The essential oil is rich in bioactive monoterpenoids such as D-limonene, β-pinene, γ-terpinene. Recently scientifically proven therapeutic activities of C. limon include anti-inflammatory, antimicrobial, anticancer and antiparasitic activities. The review pays particular attention, with references to published scientific research, to the use of C. limon in the food industry and cosmetology. It also addresses the safety of use and potential phototoxicity of the raw materials. Lastly, the review emphasizes the significance of biotechnological studies on C. limon.

A comparative metabolite analyses of the ethanolic extract of leaf and corm of Colocasia esculenta (L) schott. by GC-MS

Colocasia esculenta is a food crop and a folklore medicinal plant with high pharmacological properties. The underground corm and leaves are the edible parts of the plant. This study was aimed to characterize the bioactive metabolites in leaves and corms of C. esculenta (L) Schott. The secondary metabolites in Colocasia leaves and corms were refluxed in ethanol and the metabolites present in the ethanolic extract were analysed through gas chromatography coupled with mass spectroscopy (GC-MS). GC-MS analysis of the ethanolic extract of leaves and corms of C. esculenta revealed the presence of 25 bioactive compounds with valuable biological activities. The identification of these bioactive compounds supports the wide application of this plant as a medicine. Further research is required as the biological activities of many metabolites are yet to be reported. Also, new scientific techniques can help in using these valuable compounds in drug development for several diseases.

Characteristics of Water-soluble Polysaccharides Extracts Produced from Perilla Seed Meal via Enzymatic Hydrolysis

ABSTRACT This study was conducted to produce water-soluble polysaccharide extracts (WSP) from perilla seed meal (PSM), a by-product of perilla seed oil extraction, using enzymatic hydrolysis. The aim was to confirm the potential of this method to obtain functional materials from PSM. The cellulose and hemicellulose fractions from PSM were hydrolyzed using Celluclast 1.5 L and Viscozyme L, respectively. The yield of WSP from both fractions increased with an increase in hydrolysis time. Physical properties of WSP, including solubility, oil-holding capacity, and emulsification properties, were increased by enzymatic hydrolysis. WSP produced by hydrolysis had greater antioxidant activity than WSP obtained without hydrolysis; the highest activity was observed after a hydrolysis reaction of 24 h. WSP retarded glucose and bile acid absorption. The data indicate that WSP from PSM have potentially valuable functional and biological activities.

Production and characterization of liposomes with encapsulated bioactive soy protein hydrolysate

Soy proteins known for their high nutritional value and pronounced techno-functional properties, can be hydrolyzed by using proteolytic enzymes and thus converted into hydrolysates rich in di-, tri- and oligopeptides. The resulting peptides are carriers of valuable biological activities, which make the soy hydrolysates very important in functional food applications as techno-functional and bioactive ingredients. However, commercial incorporation and application of soy protein hydrolysates can be hinderedby their low bioavailability and instability, bitter taste, hygroscopicity and possibility to interact with the food matrix. The aim of this research is encapsulation of the soy protein hydrolysate in liposomes in order to overcome the stated shortcomings, while preserving the biological activities that protein hydrolysates exhibit. The soy hydrolysate was prepared by a two-step enzymatic hydrolysis of a soy protein concentrate using commercial food-grade proteases, endoprotease from Bacillus amyloliquefaciens (Neutrase?) and egzo- and endoprotease from Aspergillus oryzae (Flavourzyme?) and encapsulated within liposomes. The liposomes were produced by a thin film method using a commercial lipid mixture (Phospolipon? 90G) containing mainly phosphatidylcholine. Next, the obtained multilamellar vesicles (MLV) with the soy protein hydrolysate were treated by high-intensity ultrasound waves generated by using (1) an ultrasonic probe at a frequency of 20 kHz and (2) an ultrasonic bath with a frequency 40 kHz. The smallest (310 nm) and uniform (unimodal size distribution) liposomes with the highest efficiency of peptide encapsulation (19 %) were obtained by the probe sonication. The presented results showed that incorporation of the soy protein hydrolysates was achieved within the liposome membrane and caused an increase in the liposome size in all tested formulations, namely: from 297 to 310 nm by using the ultrasonic probe, from 722 to 850 nm by using the ultrasonic bath, while in formulations without the ultrasonic treatments the increase from 2818 to 3464 nm was recorded. The entrapped peptides caused enlargement of all liposomes and the increase in negative charge of zeta potential values, which in the case of MLV liposomes was below -30 mV, indicating high stability of these liposomes. Significant antioxidant activity of the probe-sonicated liposomal formulation was confirmed by the ABTS scavenging ability and iron-chelating activity. Release studies conducted under simulated gastrointestinal conditions confirmed that liposomes provide prolonged release of encapsulated soy protein hydrolysates as compared to diffusion of the free hydrolysate. In the first 75 min, only 20 % of liposome encapsulated soy peptides diffused, which is 2.2-fold lower as compared to the diffusion of the non-encapsulated soy hydrolysate. Liposome encapsulated soy protein hydrolysates may provide the possibility for application in the areas such as food science and technology, with the aim to enhance the nutritional value and shelf life of food products, and develop functional foods.

Synthesis of Azide Functionalized Tetrahydrobenzofurans and their Antineoplastic Study.

In chemistry, the derivatives of benzofuran which are substituted on five-membered ring constitute one of the salient moieties in medicinal field and a survey of literature revealed that a good number of reports have shown that tetrahydrobenzofuran derivatives are of valuable biological activities. On the basis of previous survey, we aimed to generate a series of 2-(4-azidobenzoyl)-3-substitutedaryl-6,6-dimethyl-2,3,6,7-tetrahydrobenzofuran-4(. The tetrahydrobenzofuran derivatives were synthesized by multi-component reactions. It was achieved by coupling of dimedone (3.57 mmole), 4-azido phenacyl bromide (3.92 mmole) and various aromatic aldehydes (3.57 mmole) using two different bases i.e. pyridine and. The results from anti-cancer study shows that the compound 4a exhibited diverse cytotoxic activity against renal cancer panel (UO-31) with significant selectivity and had inhibitory effect on the generation of UO-31 (growth percent= 69.36%) and the compound 4e showed comparable activity in the same cell-line (UO-31: growth percent= 80.86%). In summary, a series of azide group containing tetrahydrobenzofuran derivatives have been synthesized and were evaluated for their anticancer activity. It was concluded that the derivatives 4a and 4e exhibited promising anticancer activity. Nature of substituent on phenyl ring seems to be the crucial factor affecting the activity in both the compounds.